Studies on 3′-quaternary ammonium cephalosporins—IV. Synthesis and antibacterial activity of 3′-(2-alkyl-3-aminopyrazolium)cephalosporins related to FK037
| Autor: | Kazuo Sakane, Yoshiko Inamoto, Toshiaki Kamimura, Kohji Kawabata, Shinya Okuda, Hidenori Ohki |
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| Rok vydání: | 1997 |
| Předmět: |
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Molecular medicine.drug_class Stereochemistry Clinical Biochemistry Antibiotics Cephalosporin Substituent Pharmaceutical Science Microbial Sensitivity Tests medicine.disease_cause Biochemistry Microbiology chemistry.chemical_compound In vivo Drug Discovery medicine Ammonium Molecular Biology biology Chemistry Pseudomonas aeruginosa Organic Chemistry Ceftizoxime biology.organism_classification Anti-Bacterial Agents Cephalosporins Molecular Medicine Antibacterial activity Bacteria |
| Zdroj: | Bioorganic & Medicinal Chemistry. 5:1685-1694 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/s0968-0896(97)00092-8 |
| Popis: | The synthesis and in vitro antibacterial activity of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido] cephalosporins bearing various 2-alkyl-3-aminopyrazolium groups at the 3-position are described. Antibacterial activity against MRSA was affected by the nature of the substituent at the 2-position on the 3'-aminopyrazolium groups. Among the cephalosporins prepared in this study, 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-[3-am ino-2-(2 -hydroxyethyl)-pyrazolio]methyl-3-cephem-4-carboxylate sulfate (23e, FK037) showed extremely potent broad-spectrum activity against both Gram-positive bacteria including MRSA, and Gram-negative bacteria including Pseudomonas aeruginosa. In particular, the in vivo activity against MRSA of FK037 was the highest of all the beta-lactam antibiotics tested. |
| Databáze: | OpenAIRE |
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